GABA enhancement of flunitrazepam binding in mice selectively bred for differential sensitivity to ethanol.

Alcohol and drug research Pub Date : 1987-01-01
R J Marley, J M Wehner
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Abstract

The binding of the benzodiazepine [3H]flunitrazepam (FNZ) and the allosteric enhancement of FNZ binding by gamma-aminobutyric acid (GABA) were investigated in brain tissue from short-sleep (SS) and long-sleep (LS) mice, lines selectively bred for differential sensitivity to ethanol. GABA enhanced FNZ binding in a dose-dependent manner in both lines. This enhancement was greater in SS than in LS cortical and cerebellar regions, but did not differ between lines in midbrain or hindbrain regions. In whole brain, no difference was observed between the two lines in the number or affinity of benzodiazepine receptors, as determined by FNZ binding. These results suggest that the nature of allosteric interactions within the GABA-benzodiazepine receptor complex is different for LS and SS mice.

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GABA增强氟硝西泮与选择性饲养的乙醇敏感性差异小鼠的结合。
研究了短睡眠(SS)和长睡眠(LS)小鼠脑组织中苯二氮卓类[3H]氟硝西安定(FNZ)的结合以及γ -氨基丁酸(GABA)对FNZ结合的变构增强作用。GABA在两种细胞系中均以剂量依赖的方式增强FNZ结合。这种增强在SS区比LS皮质区和小脑区更明显,但在中脑和后脑区没有差异。在全脑中,两系之间苯二氮卓类受体的数量或亲和力没有差异,这是由FNZ结合决定的。这些结果表明,gaba -苯二氮卓受体复合物内变构相互作用的性质在LS和SS小鼠中是不同的。
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